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Synthesis and Evaluation of Neutral Phosphate Triester Backbone-Modified siRNAs.
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-06-09 , DOI: 10.1021/acsmedchemlett.0c00232
Kouta Tsubaki 1, 2 , Matthew L Hammill 2 , Andrew J Varley 2 , Mitsuru Kitamura 1 , Tatsuo Okauchi 1 , Jean-Paul Desaulniers 2
Affiliation  

Two unsymmetrical dinucleotide phosphate triesters were synthesized via transesterification from tris(2,2,2-trifluoroethyl) phosphate. The protected triesters were phosphytilated to generate phosphoramidites for solid-phase oligonucleotide synthesis. Neutral phenylethyl phosphate-modified short-interfering RNAs (siRNAs) were synthesized and evaluated for their gene-silencing ability, siRNA strand selection, and resistance to nucleases. These backbone-modified phosphate triester siRNAs offer many improvements compared to natural unmodified siRNAs.

中文翻译:

中性磷酸三酯骨架修饰的siRNA的合成和评估。

通过三(2,2,2-三氟乙基)磷酸酯的酯交换反应合成了两个不对称的磷酸二核苷酸三酯。使受保护的三酯磷酸化以产生亚磷酰胺以用于固相寡核苷酸合成。合成了中性磷酸苯乙基酯修饰的短干扰RNA(siRNA),并对其基因沉默能力,siRNA链选择和对核酸酶的抗性进行了评估。与未经修饰的天然siRNA相比,这些主链修饰的磷酸三酯siRNA提供了许多改进。
更新日期:2020-07-09
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